Folate‐PEG‐PROTAC Micelles for Enhancing Tumor‐Specific Targeting Proteolysis In Vivo

Author:

Ma Junhui1,Fang Lei1,Sun Zhengjun1,Li Meijing1,Fan Ting1,Xiang Guangya123,Ma Xiang12ORCID

Affiliation:

1. Department of Pharmacy Tongji Medical College Huazhong University of Science and Technology Wuhan 430030 China

2. Department of Pharmacy Tongren Polytechnic College Tongren 554300 China

3. Institute of the Higher Education Edible and Medicinal Fungi Engineering Research Center Tongren 554300 China

Abstract

AbstractProteolysis targeting chimeras (PROTACs) technology is rapidly developed as a novel and selective medicinal strategy for the degradation of cellular proteins in cancer therapy. However, the applications of PROTACs as heterobifunctional molecules are largely limited by high molecular weight, low bioavailability, poor permeability, insufficient targeting, and low efficacy in vivo. Herein, self‐assembling micelles of FA‐PEG‐PROTAC are designed for cancer cell selective targeting and reductive‐response proteolysis in tumor‐bearing mice. FA‐PEG‐PROTAC is prepared by conjugating folic acid (FA)‐PEG with EGFR‐targeting PROTAC via a disulfide bond. The FA‐PEG‐PROTAC micelles, formed by self‐assembling, are demonstrated to significantly improve tumor targeting efficacy and exhibit excellent anti‐tumor efficacy in the mouse xenograft model compared to the traditional PROTACs. The strategy of applying self‐assembled FA‐PEG‐PROTAC micelles in tumor therapy can not only improve targeted proteolysis efficiency but also broaden applications in the development of PROTAC‐based drugs.

Funder

National Natural Science Foundation of China

Publisher

Wiley

Cited by 1 articles. 订阅此论文施引文献 订阅此论文施引文献,注册后可以免费订阅5篇论文的施引文献,订阅后可以查看论文全部施引文献

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3